• The Korean Journal of Pesticide Science
• /
• v.6 no.4
• /
• pp.279-286
• /
• 2002

To improve the growth inhibition activities and selectivities for quinclorac family, novel 3-substituted phenyl-5-(3,7-dichloro-8-quinolinyl)-1,2,4-oxadiazole derivatives as the substrate were synthesized and their the activities ($pI_{50}$) against shoot and root of rice plant (Oryza sativa L.) and barn-yard grass (Echinochloa crus-galli) were measured. And the quantitative structure-activity relationships (QSARs) between physicochemical parameters of the substitutents (R) on phenyl group and the activities ($pI_{50}$) were analyzed quantitatively. According to the SAR analyses, the substrates of planar conformation showed higher herbicidal activities against barnyard grass than rice plant. The activities against rice plant depend on the electronic effect (shoots: ${\sigma}_{opt.}=0.49$ & root: $R_{opt.}=-0.15$) of substituents, whereas the activities against shoots and roots of barnyard grass depend on hydrophobicity (${\pi}_{opt.}=0.37{\sim}2.40$). There were conditions of selective growth inhibition activity against barnyard grass when such a ortho-substituted electron donating substituents showing the hydrophobicity value, ${\pi}=2.40$ were introduced on the phenyl ring. The 2-tolyl substituent predicted from SAR equations was expected to have better growth inhibition activity and selectivity (${\Delta}pI_{50}=1.26$) for barnyard grass.

• Journal of Periodontal and Implant Science
• /
• v.26 no.4
• /
• pp.1013-1021
• /
• 1996

There are many important factors in periodontal inflammation. $IL-1{\beta}$, $PGE_2$ and collagenase are predorminantly key factors. These inflammatory mediators induce gingival tissue and alveolar bone destruction. For the prevention and treatment of periodontal disease, it is necessary to inhibit $IL-1{\beta}$, $PGE_2$ production and collagenase activity. Ursodeoxycholic acid(UDCA) has immunomodulatory properties, and there is evidence that some natural extracts show antiinflammatory activity to some degree. The purpose of this study was to assess the inhibitory effect of UDCA and its mixture with natural extracts on $IL-1{\beta}$, $PGE_2$ production and collagenase activity. Accordingly we assessed the effect of UDCA and its mixture combined with some natural extracts on inhibition of $IL-1{\beta}$, $PGE_2$ production and collagenase activity. For the $IL-l{\beta}$ inhibition study, cultured cells were exposed to $25{\mu}g/ml$ LPS. $IL-1{\beta}$ activity was measured by $IL-1{\beta}$ enzyme immunoassay system. Human gingival fibroblasts were prepared and cells (l05/well) were seeded into culture plates. $rhIL-1{\beta}$ was added to induce $PGE_2$. The amount of $PGE_2$ in sample media was measured using enzyme immunoassay system. Crude collagenase was prepared from Porphyromonas gingivalis and collagenolytic activity was determined using a Collageno kit CLN-100. The test inhibitor was added to the assay mixture consisting of 0.1ml of 50mM Tris buffer(pH 7.5) and 0.2ml of substrate solution. UDCA and UDCA combined with natural extracts generally inhibited $IL-1{\beta}$ production. groups above 0.01% UDCA strongly inhibited $IL-l{\beta}$ synthesis. Both groups inhibited $IL-1{\beta}-induced$ synthesis of $PGE_2$. In low concentration, the degree of inhibition was as same as prednisolone. In high concentration, each group was superior to prednisolone. UDCA group and UDCA mixture group exerted a moderate inhibition of collagenolytic enzyme. The present study suggested that UDCA and its mixture with natural extracts could be further investigated as antiinflammatory drug for periodontal disease.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.47 no.2
• /
• pp.163-170
• /
• 2021

This study was conducted to create a technology to remove acne bacteria with human-friendly materials. First, the Cutibacterium acnes (C. acnes) were adsorbed to the mica disc to grow, and then the biofilm was checked through an atomic microscope to see if the biofilm had grown. Based on the topographic image, the shape changed round, the size was 17% longer on average, and the phase value of the resonance frequency separating materials was observed as a single value, the biofilm grown by covering the extracellular polymeric substrate (EPS). As a result of processing 50 mM of amino acids in the matured biofilm, the concentration of C. acnes decreased when valine, serine, arginine and leucine were treated. Scanning with nanoindentation and AFM contact modes confirmed that the hardness of biofilms treated with Valine (Val) increased. This indicates that an AFM tip measured cell which may have more solidity than that of EPS. The experiment of fluorescent tagged to EPS displays an existence of EPS at the condition of 10 mM Val, but an inhibition of growth of EPS at the 50 mM Val. Number of C. acnes was also reduced above 10 mM of Val. Weak adhesion of biofilm generated from an inhibition of EPS formation seems to induce decrease of C. acnes. Accordingly, we elucidated that Val has an efficiency which eliminates C. acnes by approach of an inhibition of EPS.

• Journal of Life Science
• /
• v.29 no.2
• /
• pp.164-172
• /
• 2019

In Korea, shiitake mushroom, Lentinula edodes, is cultivated on artificial medium containing oak sawdust and wheat bran. The annual production of spent mushroom substrate (SMS) of shiitake, a byproduct of the mushroom industry, is estimated to reach over 50,000 tons per year. This study aimed to improve the use of SMS as a novel bioresource. Hot water extracts of SMS after the first and third harvest were prepared and their bioactivities evaluated. Hot water extracts of uninoculated medium and shiitake were used as controls. Extracts of SMS showed higher radical scavenging of DPPH anions, ABTS cations, nitrites, and a higher reducing power than those of shiitake or medium extracts. After the first and third harvests at 0.5 mg/disc, SMS extracts showed no antibacterial or antifungal activities against the pathogenic and food-spoilage bacteria and fungi. However, they showed good inhibitory activities against ${\alpha}$-glucosidase at 0.5 mg/ml. In addition, SMS extracts had strong anti-coagulation activities via their inhibition of thrombin, prothrombin, and blood coagulation factors without platelet aggregation activity. Our results suggested SMS should no longer be perceived as a useless byproduct but should be understood as a novel bioresource, the extracts of which could be developed as antioxidant, antidiabetic, and antithrombosis agents.

• Journal of Life Science
• /
• v.28 no.3
• /
• pp.351-356
• /
• 2018

L-Serine dehydratase (LSD) is an iron-sulfur containing enzyme that catalyzes the conversion of L-serine to pyruvate and ammonia. Among the bacterial amino acid dehydratases, it appears that only the L-serine specific enzymes utilize an iron-sulfur cluster at their catalytic site. Moreover, bacterial LSDs are classified into four types based on structural characteristics and domain arrangement. To date, only the LSD enzymes from a few bacterial strains have been studied, but more detailed investigations are required to understand the catalytic mechanism of various bacterial LSDs. In this study, LSD type II from Mycobacterium tuberculosis (MtLSD) H37Rv was expressed and purified to elucidate the biochemical and catalytic properties using the enzyme kinetic method. The L-serine saturation curve of MtLSD exhibited a typically sigmoid character, indicating an allosteric cooperativity. The values of $K_m$ and $k_{cat}$ were estimated to be $59.35{\pm}1.23mM$ and $18.12{\pm}0.20s^{-1}$, respectively. Moreover, the plot of initial velocity versus D-serine concentration at fixed L-serine concentrations showed a non-linear hyperbola decay shape and exhibited a competitive inhibition for D-serine with an apparent $K_i$ value of $30.46{\pm}5.93mM$ and with no change in the $k_{cat}$ value. These results provide insightful biochemical information regarding the catalytic properties and the substrate specificity of MtLSD.

• Korean Journal of Food Science and Technology
• /
• v.15 no.1
• /
• pp.56-61
• /
• 1983

Direct production of biomass from starch using amylolytic yeast, Sporobolomyces holsaticus FRI Y-5 was studied with varying the ratios between carbon and other nutrient sources in the medium. It was investigated under condition of constant C/P and C/S ratio to influence the initial concentration of starch $(S_o)$ and C/N ratio on its growth which is described as the specific growth rate $({\mu})$, cell yield (Y), the maximum concentration of cell $(X_m)$, and productivity (P). They were very dependent on both $S_o$ and C/N ratio. The form of the relationship between and ${\mu}$ and $S_o$ was observed to be similar to saturation kinetics at C/N = 100 but presented substrate inhibition at other C/N ratios. As $S_o$ was changed from 22.5 to 90 g/l, Y was observed to vary with C/N ratios but seemed to decrease as a wholes. $X_m$ was linearly related to $S_o$ at more than C/N = 50 but at less than C/N = 10 substrate inhibition was presented. P increased suddenly to $S_o$ = 45 g/l and then changed decreasingly at less than C/N = 50, but at more than C/N = 100 it changed increasingly. The effect of C/P ratio and C/S ratio on the yeast growth was also investigated at constant $S_o$ and C/N ratio. ${\mu}$ was dependent on C/P and C/S ratios, but Y, independent on them. But $X_m$ was reliant upon C/P ratio but not upon C/S ratio.

• Applied Biological Chemistry
• /
• v.51 no.3
• /
• pp.171-176
• /
• 2008

The comparative molecular similarity indices analysis (CoMSIA) models between 3${\beta}$-Hydroxy-12-oleanen-28-oic acid (1-30) analogues as substrate molecule and their inhibitory activities ($pI_{50}$) against protein tyrosine phosphatase (PTP)-1B were derived and discussed quantitatively. Listing in order, the CoMFA>CoMSIA${\geq}$HQSAR>2D-QSAR model, these QSAR models had the better statistical values. The optimized CoMSIA F1 model at grid 3.0${\AA}$ had the best predictability and fitness ($q^2$=0.754 and $r^2$=0.976) by field fit alignment. The order of contribution ratio (%) of CoMSIA fields concerning the inhibitory activities was a H-bond acceptor (48.9%), steric field (25.8%) and hydrophobic field (25.4%), respectively. Therefore, the inhibitory activities of substrate molecules against PTP-1B were dependent upon H-bond acceptor field (A) of $R_4$-group. From the analytical results of CoMSIA contour maps, oleanolic acid derivatives will have better inhibition activities if $R_1$ group has H-bond acceptor disfavor, $R_3$group has steric disfavor and $R_4$ group has steric, hydrophobic, H-bond favor.

• Journal of the Korea Organic Resources Recycling Association
• /
• v.14 no.3
• /
• pp.126-137
• /
• 2006

Behaviors of simple organic compound and granular sludge in an upflow anaerobic sludge blanket (UASB) reactor treating propionate at high ammonia nitrogen levels were investigated for 12 months. The UASB reactor achieved about 80% removal of chemical oxygen demand (COD) at ammonia nitrogen concentration up to 6000 mg-N/L. At higher concentration of ammonia nitrogen, the propionate in the effluent increased whereas the acetate was very low. At ammonia nitrogen concentration of 8000 mg-N/L, the volatile suspended solids (VSS) increased sharply due probably to the decrease of the content of extracellular polymer (ECP) although methane production was very low. The specific methanogenic activity (SMA) using formate, acetate, and propionate as substrate to granules decreased as ammonia nitrogen concentration increased. The ammonia nitrogen concentration $I^{50}$, causing 50% inhibition of SMA were 2666, 4778 and 5572 mg-N/L, respectively. The kinetic coefficients of ammonia inhibition using formate, acetate, and propionate as substrate were 3.279, 0.999 and 0.609, respectively. The SMA using formate was severely affected by ammonia nitrogen than those using acetate and propionate. This result indicated that the hydrogenotrophic methanogens was most affected by ammonia nitrogen. Granules were mainly composed of microcolonies of methanothrix-like bacteria resembling bamboo-shape, and several other microcolonies including propionate degrader with juxtapositioned syntrophic associations between the hydrogen-producing acetogens and hydrogen-consuming methanogens.

• Korean Journal of Food Science and Technology
• /
• v.32 no.5
• /
• pp.1079-1086
• /
• 2000

Pectinesterase inhibitor(PEI) of ripened kiwi fruit(Actinidia chinensis) was separated with affinity chromatography using CNBr-activated Sepharose 4B being covalently bound by orange pectinesterse(PE). The affinity resin strongly and selectively bound PEI, which could be eluted in high yield as a single peak by pH 9.5 without loss of inhibitory activity. The separated PEI had maintained almost inhibitory activity at $-25^{\circ}C$ and $5^{\circ}C$ during 30 days but lost it at room temperature in 4 weeks. The PEI possessed a molecular weight of 16.6 KDa, as estimated by 12.5% SDS-PAGE. PEI had optimum pH of 7.5, optimum temperature of below $10^{\circ}C$ and stability up to $70^{\circ}C$. Also, optimum inhibitory activity for PEI was obtained in 0.2 M NaCl of substrate solutions. The kind of inhibition on tomato pectinesterase was found to be noncompetitive, using citrus pectin as substrate. Fresh orange juice added with crude PEI extracts maintained almost the same cloud stability as pasteurized juice. In case of apple juice, the addition of crude PEI extracts to apple juice had decrease of L-ascorbic acid with nearly no effect on cloud loss.

• Preventive Nutrition and Food Science
• /
• v.10 no.1
• /
• pp.6-10
• /
• 2005

The trypsin inhibitor activity (TIA) of various soybean cultivars was evaluated by measuring the inhibition of trypsin activity using N-benzoyl-DL-arginine-p-nitro-anilide (BAPNA) as the substrate. The TIA values of eleven white shelled soybean cultivars including a glyphosate-tolerant soybean (16.58 to 17.90㎎/g) were not significantly different among cultivars. Black shelled soybeans had higher TIA values, ranging from 40.09 to 52.11㎎/g, compared to white shelled soybeans (p<0.05). When the TIA of commercially processed soybean foods were determined, no TIA was detected in soysauce, tofu and soybean paste. During conventional moist heating, the IT/sub 50/ (Time required to reach 50% inhibition of TIA) values were decreased as heating temperature and cooking pressure increased. The IT/sub 50/ values of moist heating were estimated to be 91.68, 37.71 and 19.50 min at 60, 80 and 100℃, respectively. The IT/sub 50/ value of microwave cooking was 4.75 min at medium heat, while that of the pressure cooking at 120℃ was only 2.62min. Moreover, there was a negative relationship between temperature and IT/sub 50/ values (R=0.92, p<0.01). The TIA of soybean sprouts was completely inactivated after heating at 100℃ for 5 min, although fresh soybean sprouts showed one fifth of the TIA value of white shelled soybeans. Based on our results, pressure cooking is the most effective cooking method to reduce TIA in soybeans.